Faculty of Medicine and Health Technology, Tampere University, Arvo Ylpön katu 34, FI-33520 Tampere, Finland.
Neurofarba Department, Sezione di Chimica Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Via U. Schiff 6, I-50019 Sesto Fiorentino (Firenze), Italy.
J Inorg Biochem. 2020 Dec;213:111274. doi: 10.1016/j.jinorgbio.2020.111274. Epub 2020 Oct 7.
The protozoan pathogen Trichomonas vaginalis encodes two carbonic anhydrases (CAs, EC 4.2.1.1) belonging to the β-class. One of these enzymes, T. vaginalis carbonic anhydrase 1 (TvaCA1), was recently cloned and characterized by our group, and its X-ray crystal structure reported. No inhibitors of this enzyme were reported up until now. Here we investigated the inhibition of TvaCA1 with inorganic anions and small molecules and observed that thiocyanate, cyanide, selenite, selenocyanate and divanadate are sub-millimolar inhibitors, whereas sulfamide, sulfate, phenylboronic acid and phenylarsonic acid are micromolar inhibitors. Finding effective TvaCA1 inhibitors may be useful for developing new antiprotozoan drugs.
原生动物病原体阴道毛滴虫编码两种属于β类的碳酸酐酶（CA，EC 4.2.1.1）。我们小组最近克隆并表征了其中一种酶，即阴道毛滴虫碳酸酐酶 1（TvaCA1），并报道了其 X 射线晶体结构。到目前为止，还没有报道这种酶的抑制剂。在这里，我们研究了无机阴离子和小分子对 TvaCA1 的抑制作用，发现硫氰酸盐、氰化物、亚硒酸盐、硒氰酸盐和偏钒酸盐是亚毫摩尔抑制剂，而磺胺、硫酸盐、苯硼酸和苯胂酸是毫摩尔抑制剂。找到有效的 TvaCA1 抑制剂可能有助于开发新的抗原生动物药物。
